antihyperlipidemic therapies Flashcards
coronary heart disease causes what amount of deaths in us?
half
incidence of chd correlates with what?
high levels of ldl, cholesterol, and triacylglycerols
low levels of hdl cholesterol
risk factors for chd include?
cigarette smoking, htn, obesity, diabetes, family hx
therapies aim to do what 3 things?
- decrease carrier production
- increase degradation
- decrease absorption
- increase removal
Hyperlipidemias have been classified into __ major subtypes*
Coronary heart disease (CHD) causes ___ of all deaths in US
The most common types of hyperlipidemias involve elevated LDL (____)
HYPERLIPIDEMIA
Hyperlipidemias have been classified into 5 major subtypes*
Coronary heart disease (CHD) causes 1/2 of all deaths in US
The most common types of hyperlipidemias involve elevated LDL (IIa)
build up of lipids on periphery or cornea
arcus sinilis
related to ldl (cholesterol)
type 4 (VLDL)
triglycerol
anti hyperlipidemic therapies
decrease carrier production
increase degradation
decrease absorption
increase removal
lipids are not water soluble therefore
they need to be placed in something that is so they can float around (proteins); markers are on proteins
site of cholesterol production
liver
where do we absorb lipids?
GI
where do we remove lipids?
packaged by liver –> deposited in bile pathway –> GI –> removed by feces
or
water soluble substance –> urine
high lipid develop into
artherosclerosis
high lipid is reflected in eye by what?
hollenhorst plaque
which cholesterol is the good one?
hdl
6 drug classes for antihyperlipidemic drug
HMG CoA Reductase Inhibitors (Statins) Fibrates Niacin Cholesterol Absorption Inhibitors Bile Acid Sequestrants Omega-3 Fatty Acids
3 most pops AHD classes?
HMG CoA Reductase Inhibitors (Statins)
Fibrates
Niacin
best selling hmg coa reductase inhibitor
atorvastatin (lipitor)
first hmg coa inhibitor on the market
lovastatin
which drug: derived from red rice yeast –> fungus –> protects
lovastatin
long acting hmg coa ri
atorvastatin
short acting hmg coa ri
simvastatin; wont cause as many complications to bod
INDICATION
Hyperlipidemia/CVD Prevention
DOSING [10-80mg]
1 tabs qd
ATORVASTATIN
taken at night while body is at rest
atorvastatin
CLINICAL PHARMACOLOGY
Antihyperlipidemic/Antidyslipidemic
Mechanism of Action
Competitively inhibits HMG-CoA Reductase which is responsible for an early, rate-limiting step in cholesterol biosynthesis
Increases hepatic LDL receptors, enhancing catabolism
atorvastatin moa
ocular side effect thats most criticized when taking statins
cataracts
Common: nasopharyngitis, myalgia
Skeletal: myopathy
Hepatic: impaired function associated w/ elevated serum transaminase levels; jaundice
CNS: amnesia
Ocular: diplopia, ptosis, pseudo-CME, blurred vision, elevated IOP, intraocular hemorrhage, cataracts*
atorvastatin
diabetics with statins
more at risk for developing cataracts
least significant side effects of statins are:
simvastatin and pravastatin
when taking atorvastatin with cyclocporine or if taken for a long time, whats a developed side effect?
muscle pain (myopathy exacerbation)
2 types of fibrates
Fenofibrate [Tricor®, Lofibra®, Triglide®]
Gemfibrozil [Lopid®]
top selling fibrate
fenofibrate
INDICATION
Hypertriglyceridemia, Hypercholesterolemia
DOSING [48/145 mg]
48-145 mg qd
fenofibrate
CLINICAL PHARMACOLOGY
Fibrates
Mechanism of Action
Stimulates nuclear receptor PPAR which modulates transcription of insulin sensitive genes in liver, muscle and adipose tissue
Enhances HDL production; inhibits triglyceride synthesis and stimulates catabolism of triglyceride-rich lipoproteins
fenofibrate
what insulin reponsible for?
pulling glucose out of blood; fat metabolism
Nicotinic Acid [Vitamin B3, Niacin, Niaspan®, Slo-Niacin®]
niacin
INDICATION
Hypertriglyceridemia, Hypercholesterolemia, Mixed Dyslipidemia
DOSING [50-1000 mg]
1500-3000 mg/d
niacin
CLINICAL PHARMACOLOGY
Vitamins/Nutritionals
Mechanism of Action
Inhibits lipolysis in adipose tissue, resulting in reduced hepatic VLDL synthesis and production of LDLs in the plasma
moa of niacin
dose of niacin
1500-3000 mg/d **HUGE
a pt is on glaucoma therapy, which drug is contraindicated due to additive hypotension
niacin
